Albiglutide

Catalog No.S3734

Albiglutide Chemical Structure

Molecular Weight(MW): 3283.6

Albiglutide is a glucagon-like peptide-1 agonist (GLP-1 agonist).

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Biological Activity

Description Albiglutide is a glucagon-like peptide-1 agonist (GLP-1 agonist).
Targets
GLP-1R [1]
()
In vitro

Albiglutide is a recombinant fusion protein consisting of two copies of a 30-amino-acid sequence of modified human GLP-1 (fragment 7-36), modified with a glycine substituted for the naturally occurring alanine at position 8 in order to augment resistance to DPP-4[1].

In vivo Glucose lowering occurs within 24 h after a single dose of albiglutide, as a result of binding of the molecule to the GLP-1 receptor. The reduction in both fasting and postprandial glucose levels is dose related. Albiglutide is less potent than GLP-1. In animal models of diabetes, albiglutide administration stimulates increased β-cell mass. Following SC administration of a single 30-mg dose to patients with type 2 diabetes, maximum concentration is reached in 3-5 days with half-life of 3.6-6.8 days. The apparent volume of distribution after a single dose of albiglutide was 8.2-18.5 L. The eventual fate of albiglutide in the circulation is degradation into small peptides and individual amino acids. Albiglutide had no apparent effects on cardiovascular function, heart rate, electrocardiographic intervals, or respiratory function and did not produce any evidence of electrocardiographic abnormalities or arrhythmias in male cynomolgus monkeys. Furthermore, there were no albiglutide-related effects on neurobehavioral functional assessments. Albiglutide does not cross the blood–brain barrier to reach the satiety centers[1]. Albiglutide reduced myocardial infarct size and improved cardiac function and energetics following myocardial I/R injury which are associated with enhanced myocardial glucose uptake and a shift toward a more energetically favorable substrate metabolism by increasing both glucose and lactate oxidation[2].

Protocol

Animal Research:

[2]

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  • Animal Models: Male Sprague-Dawley rats
  • Formulation: --
  • Dosages: 1, 3 or 10 mg/kg/day
  • Administration: s.c.
    (Only for Reference)

Solubility (25°C)

In vitro Water 100 mg/mL (30.45 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 3283.6
Formula

C148H224N40O45

CAS No. 782500-75-8
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03015519 Withdrawn Drug: Albiglutide|Drug: Placebo Diabetes Mellitus Type 2 GlaxoSmithKline August 14 2017 Phase 3
NCT02750930 Terminated Drug: Albiglutide|Device: Auto-injector Diabetes Mellitus Type 2 GlaxoSmithKline October 7 2016 Phase 4
NCT02229227 Completed Drug: Albiglutide|Drug: Insulin Glargine and Insulin Lispro Diabetes Mellitus Type 2 GlaxoSmithKline|PPD November 21 2014 Phase 3
NCT01475734 Completed Biological: albiglutide|Biological: placebo Diabetes Mellitus Type 2 GlaxoSmithKline December 2011 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID